N1-(2,2,6,6-tetraMethylpiperidin-4-yl)-N2-p-tolyloxalaMide

N1-(2,2,6,6-tetraMethylpiperidin-4-yl)-N2-p-tolyloxalaMide Property

Density 

1.11±0.1 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

Limited solubility

form 

Powder

pka

11.61±0.70(Predicted)

color 

White to off-white

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

H400Very toxic to aquatic life

H410Very toxic to aquatic life with long lasting effects

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P271Use only outdoors or in a well-ventilated area.

P273Avoid release to the environment.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P321Specific treatment (see … on this label).

P330Rinse mouth.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P391Collect spillage. Hazardous to the aquatic environment

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

N1-(2,2,6,6-tetraMethylpiperidin-4-yl)-N2-p-tolyloxalaMide Chemical Properties,Usage,Production

Uses

YYA-021 is a small molecule CD4 mimic HIV entry inhibitor that can suppress competitively the interaction between an HIV-1 envelope glycoprotein gp120 and a cellular surface protein CD4.

Biological Activity

yya-021 is a small-molecule cd4 mimic that inhibits hiv entry [1].cd4 is a cell surface protein. the entry of human immunodeficiency virus type 1 (hiv-1) into target cells is initiated by the interaction of cd4 and viral envelope glycoprotein gp120. cd4 mimic inhibits the interaction between gp120 and cd4 and then inhibits hiv entry [1].yya-021 is a small-molecule cd4 mimic that inhibits hiv entry. yya-021 competitively inhibited gp120-cd4 interaction [1]. in tzm-bl cells infected with simian-human immunodeficiency virus isolate mna (shiv mna) or hiv-1 mna pseudotyped viruses, yya-021 inhibited the entry of envs of shiv mna and hiv-1. kd-247 (the anti-v3 loop mab, 50 μg) caused 50% neutralization of hiv-1 mna. however, in the presence of 20 μm of yya-021, kd-247 (<0.05 μg) caused 50% neutralization of hiv-1 mna, which suggested that the synergistic neutralization effect of yya-021 and kd-247. in the presence of yya-021, shiv mna became more sensitive to igg [2].in jcl:sd rats, the maximum tolerated dose of yya-021.hcl was 2.5 mg. when administrated by tail vein injection, yya-021 exhibited widespread tissue distribution due to its hydrophobicity. in a rhesus macaque, the maximum tolerated dose of yya-021.hcl was 35.3 mg [1].

target

gp120-CD4 interaction

References

[1]. hashimoto c, narumi t, otsuki h, et al. a cd4 mimic as an hiv entry inhibitor: pharmacokinetics. bioorg med chem, 2013, 21(24): 7884-7889.
[2]. otsuki h, hishiki t, miura t, et al. generation of a replication-competent simian-human immunodeficiency virus, the neutralization sensitivity of which can be enhanced in the presence of a small-molecule cd4 mimic. j gen virol, 2013, 94(pt 12): 2710-2716.